etravirine (Intelence)
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Indications
- NNRTI for treatment of advanced HIV-1 infection (treatment-experienced adults with HIV1)
- administer with: ritonavir-bloosted darunavir or ritonavir-bloosted saquiunavir
- ok with raltegravir
- ok with maraviroc, dose of maraviroc
- 600 mg BID without HIV protease inhibitor
- 150 mg BID with HIV protease inhibitor
Contraindications
- concurrent use of
- all unboosted HIV protease inhibitors
- ritonavir-boosted tipranavir
- fosamprenavir
- use during pregnancy (data insufficient)[4]
Dosage
Tablets: 100 mg
Storage
- store in orginal container
- must be protected from moisture
- original container has a desiccant[5]
Pharmacokinetics
- hepatically metabolized by Cyt P4503A4
- also induces Cyt P450 3A4
- inhibits Cyt P450 2C9 & Cyt P450 2C19
Monitor
Adverse effects
- nausea[6]
- Stevens-Johnson syndrome
- toxic epidermal necrolysis & erythema multiforme
- hypersensitivity reactions characterized by
- rash
- constitutional findings
- sometimes organ dysfunction, including hepatic failure[2]
- drug adverse effects of antiretroviral agents
- drug adverse effects of non-nucleoside reverse transcriptase inhibitors (NNRTI)
Drug interactions
- drugs that induced or inhibit Cyt P450 3A4 or are metabolized by Cyt P450 3A
- drugs metabolized Cyt P450 2C9 & Cyt P450 2C19 may increase in concentration
Laboratory
Mechanism of action
- non-nucleoside reverse transcription inhibitor (NNRTI)
Notes
- Manufacturer: Tibotec
- cost 2008 $22/day
More general terms
References
- ↑ Prescriber's Letter 16(2): 2009 New Drugs Approved by the FDA in 2008 Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=250213&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 2.0 2.1 FDA MedWatch, 08/27/2009 http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm180579.htm
- ↑ 3.0 3.1 Prescriber's Letter 17(7): 2010 Recommended Lab Monitoring for Common Medications Liver Function Test Scheduling Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=260704&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 4.0 4.1 Zuger A Use of Antiretroviral Drugs in Pregnancy. Physician's First Watch, April 22, 2014 David G. Fairchild, MD, MPH, Editor-in-Chief Massachusetts Medical Society http://www.jwatch.org
Panel on Treatment of HIV-Infected Pregnant Women and Prevention of Perinatal Transmission. Recommendations for use of antiretroviral drugs in pregnant HIV-1-infected women for maternal health and interventions to reduce perinatal HIV transmission in the United States. 2014. AIDSinfo. Clinical Guidelines Portal. March 28, 2014. http://aidsinfo.nih.gov/Guidelines/HTML/3/perinatal-guidelines/0 (corresponding NGC guideline withdrawn March 2016) - ↑ 5.0 5.1 Prescriber's Letter 21(6): 2014 Oral Meds to Keep in Original Containers Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=300622&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 6.0 6.1 Medical Knowledge Self Assessment Program (MKSAP) 17, American College of Physicians, Philadelphia 2015
- ↑ Intelence (etravirine) tablets [prescribing information] NJ Tibotec Inc, 2008 http://www.intelence-info.com